fascaplysin [Ligand Id: 5969] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL602937 (Fascaplysin)
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • butyrylcholinesterase/Butyrylcholinesterase in Human [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Non-competitive inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate by Lineweaver-Burk reciprocal plot analysis B 5.64 pKi 2280 nM Ki Medchemcomm (2012) 3: 1098-1103
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate after 30 mins by Ellman's method B 5.83 pIC50 1490 nM IC50 Medchemcomm (2012) 3: 1098-1103
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition by Ellman's method B 5.82 pIC50 1500 nM IC50 J Med Chem (2021) 64: 1392-1422 [PMID:33528252]
butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
ChEMBL Inhibition of BuChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition by Ellman's method B 4.05 pIC50 90000 nM IC50 J Med Chem (2021) 64: 1392-1422 [PMID:33528252]
cyclin dependent kinase 4/CDK4/Cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038472] [GtoPdb: 1976] [UniProtKB: P11802P30281]
ChEMBL Inhibition of CDK4/cyclin-D3 (unknown origin) B 4 pIC50 >100000 nM IC50 Medchemcomm (2012) 3: 1098-1103
GtoPdb CDK4/cyclin D1 complex - 6.46 pIC50 350 nM IC50 Biochem Biophys Res Commun (2000) 275: 877-84 [PMID:10973815]
cyclin dependent kinase 6/CDK6/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111455] [GtoPdb: 1978] [UniProtKB: P24385Q00534]
ChEMBL Inhibition of CDK6/cyclin-D1 (unknown origin) B 5.47 pIC50 3400 nM IC50 Medchemcomm (2012) 3: 1098-1103
cyclin dependent kinase 6/CDK6/cyclin D2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301386] [GtoPdb: 1978] [UniProtKB: P30279Q00534]
ChEMBL Inhibition of CDK6/cyclin-D2 (unknown origin) B 4.3 pIC50 >50000 nM IC50 Medchemcomm (2012) 3: 1098-1103
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Non-competitive inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate by Lineweaver-Burk reciprocal plot analysis B 4.31 pKi 48490 nM Ki Medchemcomm (2012) 3: 1098-1103
ChEMBL Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate after 30 mins by Ellman's method B 4.04 pIC50 90470 nM IC50 Medchemcomm (2012) 3: 1098-1103
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493P14635]
ChEMBL Inhibition of CDK1/cyclin-B (unknown origin) B 4 pIC50 >100000 nM IC50 Medchemcomm (2012) 3: 1098-1103
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864P24941]
ChEMBL Inhibition of CDK2/cyclin-E (unknown origin) B 4.3 pIC50 >50000 nM IC50 Medchemcomm (2012) 3: 1098-1103
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802P24385]
ChEMBL Inhibition of CDK4/cyclin-D1 (unknown origin) B 6.46 pIC50 350 nM IC50 Medchemcomm (2012) 3: 1098-1103
GtoPdb CDK4/cyclin D1 complex - 6.46 pIC50 350 nM IC50 Biochem Biophys Res Commun (2000) 275: 877-84 [PMID:10973815]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301385] [GtoPdb: 1976] [UniProtKB: P11802P30279]
ChEMBL Inhibition of CDK4/cyclin-D2 (unknown origin) B 4 pIC50 >100000 nM IC50 Medchemcomm (2012) 3: 1098-1103
GtoPdb CDK4/cyclin D1 complex - 6.46 pIC50 350 nM IC50 Biochem Biophys Res Commun (2000) 275: 877-84 [PMID:10973815]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
ChEMBL Inhibition of CDK5/p-35 (unknown origin) B 4.7 pIC50 20000 nM IC50 Medchemcomm (2012) 3: 1098-1103

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]